产品
编 号:F375500
分子式:C25H24ClN3O3S
分子量:481.99
产品类型
结构图
CAS No: 515141-51-2
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产品详情
生物活性:
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity.
体内研究:
GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls.GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t1/2=11 h) and brain penetration (6:1 brain:plasma concentration) in mice.Animal Model:High fat diet-induced obese AKR/J mice
Dosage:0.3, 3, and 15 mg/kg
Administration:Orally, qd,12 days
Result:Caused a sustained dose-dependent weight loss of -6.2%, -12.1%, and -13.1%, respectively, relative to vehicle controls.
体外研究:
GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50 value of ~13?nM.